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    PROCESS FOR PREPARING CARBOXYLIC ACID AMIDES USEFUL IN THE TREATMENT OF MUSCULAR DISORDERS
    3.
    发明申请
    PROCESS FOR PREPARING CARBOXYLIC ACID AMIDES USEFUL IN THE TREATMENT OF MUSCULAR DISORDERS 有权
    制备用于治疗肌肉疾病的羧酸的方法

    公开(公告)号：US20120101301A1

    公开(公告)日：2012-04-26

    申请号：US13254409

    申请日：2010-03-03

    申请人： David Selwood

    发明人： David Selwood

    IPC分类号： C07C231/14

    CPC分类号： C07C231/02 ,  C07C231/12 ,  C07C233/69

    摘要： The present invention relates to a process for preparing a compound of formula wherein: R2 is cycloalkyl or alkyl, each of which may be optionally substituted; Y is —CONR3R4, —CN or CO2R5; R3, R4 and R5 are each independently H or alkyl; n is 1 to 6; wherein said process comprising the steps of: (i) treating a compound of formula (IV), where R1 is alkyl, with a compound of formula (V) and forming a compound of formula (IIIb); (ii) treating said compound of formula (IIIb) with a compound of formula (I1) to form a compound of formula (I).

    摘要翻译： 本发明涉及制备下式化合物的方法：其中：R 2是环烷基或烷基，其中每一个可以被任选取代; Y是-CONR 3 R 4，-CN或CO 2 R 5; R3，R4和R5各自独立地为H或烷基; n为1至6; 其中所述方法包括以下步骤：（i）将式（Ⅳ）化合物（其中R 1为烷基）与式（Ⅴ）化合物反应并形成式（IIIb）化合物; （ii）用式（I1）化合物处理式（IIIb）化合物以形成式（I）化合物。

    Modulator
    9.
    发明授权
    Modulator 有权
    调制器

    公开(公告)号：US07696382B2

    公开(公告)日：2010-04-13

    申请号：US10590064

    申请日：2005-02-21

    申请人： Masahiro Okuyama ,  David Selwood ,  Cristina Visintin ,  David Baker ,  Gareth Pryce

    发明人： Masahiro Okuyama ,  David Selwood ,  Cristina Visintin ,  David Baker ,  Gareth Pryce

    IPC分类号： C07C233/00 ,  C07C229/00 ,  C07C255/00 ,  A01N37/18

    CPC分类号： C07C235/42 ,  A61K31/165 ,  C07C69/76 ,  C07C69/78 ,  C07C233/11 ,  C07C233/65 ,  C07C233/66 ,  C07C233/69 ,  C07C235/34 ,  C07C235/78 ,  C07C235/84 ,  C07C237/32 ,  C07C237/38 ,  C07C237/42 ,  C07C255/41 ,  C07C255/44

    摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C≡—C—(CH2)2CO2H, meta-C≡—C—(CH2)2OH, meta-C≡C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C≡C—(CH2)4OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为OR 1或NR 1 R 2，其中R 1和R 2各自独立地为H或烃基; X是亚烷基，亚烯基或亚炔基，其各自可以任选地被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO2，CN，COR3，COOR3，NR3R4，CONR3R4，SO3H，SO2-R3，SO2NR3R4和CF3的极性官能团，其中R3和R4各自独立地为H或烃基; A是芳基或杂芳基，其各自可以任选被取代; 和B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A是苯基时，n是0，Z是OH，X-Y不是间位-C≡-C-（CH 2）2 CO 2 H，间-C≡C-（CH 2） （CH 2）2 CO 2 Me，间 - （CH 2）4 CO 2 H，邻-CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - （CH 2）4 CO 2 H; 和（ii）当A是苯基时，n是0，Z是OMe，X-Y不是间位-C≡C-（CH 2）4 OH。 本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。